2. PROTAC Stem Cell/Wnt Cell Cycle/DNA Damage
  3. PROTACs Casein Kinase
  4. WH-10417-099

WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
(Pink: PI3Kγ ligand (HY-168319); Blue: Cereblon ligand (HY-41547); Black: linker (HY-115384)).

For research use only. We do not sell to patients.

WH-10417-099

WH-10417-099 Chemical Structure

CAS No. : 2769753-42-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

WH-10417-099 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CK1 CK2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647)[1][2]. (Pink: PI3Kγ ligand (HY-168319); Blue: Cereblon ligand (HY-41547); Black: linker (HY-115384)).

IC50 & Target[1]

Cereblon

 

CK1

 

In Vitro

WH-10417-099 (1 μM; 1 hour) induces significant bio-ubiquitylation of 8 kinases (STK4, STK35, GSPT1, RIPK2, MAP4K4, STK3, CSNK1D, CSNK1A1) and 1 non-kinase (CSNK1E) in 293TCRBN−/− cells expressing CRBN-BirA and A3-ubiquitin, with only CSNK1E undergoing significant degradation[1].
WH-10417-099 (100 nM; 24 h) treatment of HEK293T cells drives significant downregulation of 14 proteins, including nine kinases, and co-treatment with 10 µM SB-405483 refines this subset of downregulated proteins to a stringent group of shared targets[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WH-10417-099 Related Antibodies
Molecular Weight

1039.16

Formula

C52H62N8O13S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C2CCC(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCOCCOCCOCCOCCC(NCCCN(C4CC4)S(C5=CC=C(C6=CN=C(N)C(C7=CC(CCNC8=O)=C8C=C7)=C6)C=C5)(=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (38.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9623 mL 4.8116 mL 9.6232 mL
5 mM 0.1925 mL 0.9623 mL 1.9246 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.14%

SDS (251 KB)

COA (243 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9623 mL 4.8116 mL 9.6232 mL 24.0579 mL
5 mM 0.1925 mL 0.9623 mL 1.9246 mL 4.8116 mL
10 mM 0.0962 mL 0.4812 mL 0.9623 mL 2.4058 mL
15 mM 0.0642 mL 0.3208 mL 0.6415 mL 1.6039 mL
20 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2029 mL
25 mM 0.0385 mL 0.1925 mL 0.3849 mL 0.9623 mL
30 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8019 mL
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WH-10417-099 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WH-10417-0992769753-42-4PROTACsCasein KinaseCSNK1A1E3 ubiquitin ligaseSTK35CSNK1DSTK3CRBNRIPK2STK4MAP4K4GSPT1Inhibitorinhibitorinhibit

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